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Synthesis and Biological Activity of 28-Amide Derivatives of 23-Hydroxy Betulinic Acid as Antitumor Agent Candidates

[ Vol. 9 , Issue. 7 ]

Author(s):

Yi Bi, Jinyi Xu, Fei Sun, Xiaoming Wu, Wencai Ye, Yijun Sun and Wenwen Huang   Pages 920 - 925 ( 6 )

Abstract:


Based on the structure of 23-hydroxybetulinic acid (1), a series of 28-amide derivatives were synthesized. Biological evaluation in vitro for their antitumor activities against five cell lines (A549, BEL-7402, SF-763, B16 and HL-60) has indicated that compound 6g possesses the most effective antitumor activity with an IC50 value of 10.47 μM when treated with HL-60 cells. In vivo testing has also shown a comparable activity of 6g to cyclophosphamide against H22 liver tumor in mice and 5-fluorouracil against B16 melanoma, respectively.

Keywords:

23-hydroxy betulinic acid, 28-carboxylic acid, amide derivatives, antitumor activity.

Affiliation:

Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing, 210009 Jiangsu, China and Center for Drug Discovery, College of Pharmacy, China Pharmaceuticcl University, Nanjing, 210009 Jiangsu, China.



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